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A single amino acid exchange inverts susceptibility of related receptor tyrosine kinases for the ATP-site inhibitor STI-571

Böhmer, F.D. and Karagyozov, L. and Uecker, A. and Serve, H. and Botzki, A. and Mahboobi, Siavosh and Dove, Stefan (2003) A single amino acid exchange inverts susceptibility of related receptor tyrosine kinases for the ATP-site inhibitor STI-571. The Journal of Biological Chemistry 278 (7), pp. 5148-5155.

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Other URL: http://www.jbc.org/cgi/content/full/278/7/5148


Abstract

The tyrosine kinase inhibitor STI-571 potently blocks BCR-Abl, platelet-derived growth factor (PDGF) a- and b-receptors, and c-Kit kinase activity. However Flt3, a receptor tyrosine kinase closely related to PDGF receptors and c-Kit, is not inhibited by STI-571. Sequence alignments of different kinases and indications from the crystal structure of the STI-571 Abl kinase complex revealed amino ...

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Item Type:Article
Date:2003
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Projects:Deutsche Krebshilfe 10-2100
Identification Number:
ValueType
2003:106662Other
Subjects:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
600 Technology > 610 Medical sciences Medicine
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Partially
Owner: Prof. Dr. Stefan Dove
Deposited On:20 Jan 2009 18:18
Last Modified:05 Aug 2009 13:49
Item ID:5392
Owner Only: item control page
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